Cyclosporin

Immunomodulator · Immunosuppressant

Indications

Immunosuppression in organ and bone marrow transplantation; prophylaxis and treatment of graft versus-host disease. Short term treatment of severe atopic dermatitis where conventional therapy ineffective or inappropriate. Severe psoriasis, severe eczema, severe active rheumatoid arthritis where conventional therapy ineffective or inappropriate.

Dosage

Organ transplantations: Used alone, Adults & Children over 3 mth: 10-15 mg/kg by mouth 4-12 yr before transplantations followed by 10-15 mg/kg daily for 1-2 wk postoperatively then reduced gradually to 2-6 mg/kg daily for maintenance (dose should be adjusted according to blood-cyclosporin concentration and renal function); dose lower if given concomitantly with other immunosuppressant therapy; if necessary one-third corresponding oral dose can be given by IV infusion over 2-6 hr. Bone marrow transplantation; prophylaxis and treatment of graft versus-host disease: Adults & Children over 3 mth: 3-5 mg/kg daily by IV infusion over 2-6 hr from day before transplantation to 2 wk postoperatively (or 12.5-15 mg/kg daily by mouth) then 12.5 mg/kg daily by mouth for 3-6 mth then tailed off (may take up to a yr after transplantation). Nephrotic syndrome: Adults: Orally, 5 mg/kg daily in 2…

Administration

For IV infusion only. Administer as a slow IV infusion over approximately 2-6 hours. Reconstitution: Immediately before use, dilute 1 mL of cyclosporine IV concentrate in 20-100 mL of NaCl 0.9% injection or dextrose 5% injection. Stability: Store at temperature below 30°C (86°F) and protect from light. Discard diluted infusion solutions after 24 hours.

Adverse Effects

Hyperlipidaemia, hyper-uricaemia, hyperkalaemia, hypomagnesaemia, tremor, headache, paraesthesia, hypertension (discontinue if cannot control), GI upset, anorexia, abdominal pain, gingival hypertrophy, hepatic and renal dysfunction, hypertrichosis, muscle cramps, myalgia, fatigue, anaemia, thrombocytopenia, signs of encephalopathy, rash, oedema, weigh gain, malignancies, Iymphoproliferative disorders, infections. Rarely, micro-angiopathic Haemolytic anaemia or haemolytic uraemic syndrome, menstrual disturbances, gynaecomastia, hyperglycaemia, motor polyneuropathy, pancreatitis, muscle weakness, myopathy, optic disc oedema. Risk of benign intracranial hypertension; investigate patients presenting with signs of raised intracranial pressure, withdraw cyclosporin if diagnosed.

Risk Factor (Pregnancy/Lactation)

Contraindications: Lactation. Precautions: Closely monitor renal and liver functions, BP and serum lipids. Hyperkalaemia, hyper-uricaemia, hypomagnesaemia. Avoid excess exposure to UV light. Acute untreated infection. Elderly. Pregnancy.

Interactions

Tacrolimus, other immunosuppressants, barbiturates, carbamazepine, oxcarbazepine, primidone, phenytoin, griseofulvin, trimethoprim, rifampicin, octreotide, orlistat, St. John's Wort, macrolides, azole antifungals, calcium channel blockers, metoclopramide, oral contraceptives, danazol, allopurinol, amiodarone, ursodeoxycholic acid, protease inhibitors, imatinib, nephrotoxic drugs, NSAIDs, vaccines, digoxin, corticosteroids, statins, etoposide, colchicine, K+-sparing diuretics, K+ supplement, ACE inhibitors, angiotensin II antagonists, grapefruit juice, methotrexate, H2 blockers, propafenone, bromocriptine, doxycycline, chloroquine, sulfinpyrazone, terbinafine, bosentan, substrates of CYP3A4 and/or P-qlycoprotein, repaglinide.

Pharmacokinetics

Absorption: Oral: Slow and incomplete. Metabolism: Intestinal. Hepatic. Half-life elimination: 5-27 hrs. Time to peak, plasma: 1-8 hrs. Excretion: Faeces (major). Urine (minor).

Brands with this active ingredient

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